PT1652520E - Formulations useful in the treatment of male and female impotence - Google Patents
Formulations useful in the treatment of male and female impotence Download PDFInfo
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- PT1652520E PT1652520E PT05025314T PT05025314T PT1652520E PT 1652520 E PT1652520 E PT 1652520E PT 05025314 T PT05025314 T PT 05025314T PT 05025314 T PT05025314 T PT 05025314T PT 1652520 E PT1652520 E PT 1652520E
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- Prior art keywords
- treatment
- male
- impotence
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- 238000011282 treatment Methods 0.000 title claims abstract description 13
- 239000000203 mixture Substances 0.000 title abstract description 9
- 201000001881 impotence Diseases 0.000 title description 12
- 238000009472 formulation Methods 0.000 title description 3
- 206010057671 Female sexual dysfunction Diseases 0.000 claims abstract description 5
- 206010057672 Male sexual dysfunction Diseases 0.000 claims abstract description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 3
- 239000003814 drug Substances 0.000 claims description 9
- KJPRLNWUNMBNBZ-QPJJXVBHSA-N (E)-cinnamaldehyde Chemical compound O=C\C=C\C1=CC=CC=C1 KJPRLNWUNMBNBZ-QPJJXVBHSA-N 0.000 claims description 4
- AXMVYSVVTMKQSL-UHFFFAOYSA-N UNPD142122 Natural products OC1=CC=C(C=CC=O)C=C1O AXMVYSVVTMKQSL-UHFFFAOYSA-N 0.000 claims description 4
- KJPRLNWUNMBNBZ-UHFFFAOYSA-N cinnamic aldehyde Natural products O=CC=CC1=CC=CC=C1 KJPRLNWUNMBNBZ-UHFFFAOYSA-N 0.000 claims description 4
- 229940117916 cinnamic aldehyde Drugs 0.000 claims description 4
- VNONINPVFQTJOC-ZGXDEBHDSA-N dioscin Chemical compound O([C@@H]1[C@@H](CO)O[C@H]([C@@H]([C@H]1O)O[C@H]1[C@@H]([C@H](O)[C@@H](O)[C@H](C)O1)O)O[C@@H]1CC2=CC[C@H]3[C@@H]4C[C@H]5[C@@H]([C@]4(CC[C@@H]3[C@@]2(C)CC1)C)[C@@H]([C@]1(OC[C@H](C)CC1)O5)C)[C@@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@H]1O VNONINPVFQTJOC-ZGXDEBHDSA-N 0.000 claims description 4
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- VNONINPVFQTJOC-RXEYMUOJSA-N Collettiside III Natural products O([C@@H]1[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@H](O)[C@@H](O)[C@H](C)O2)[C@H](CO)O[C@@H]1O[C@@H]1CC=2[C@@](C)([C@@H]3[C@H]([C@H]4[C@@](C)([C@H]5[C@H](C)[C@@]6(O[C@H]5C4)OC[C@H](C)CC6)CC3)CC=2)CC1)[C@H]1[C@H](O)[C@H](O)[C@@H](O)[C@H](C)O1 VNONINPVFQTJOC-RXEYMUOJSA-N 0.000 claims description 3
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- CJNUQCDDINHHHD-APRUHSSNSA-N dioscin Natural products C[C@@H]1CC[C@@]2(OC1)O[C@H]3C[C@H]4[C@@H]5CC=C6C[C@H](CC[C@@H]6[C@H]5CC[C@]4(C)[C@H]3[C@@H]2C)O[C@@H]7O[C@H](CO)[C@@H](O[C@@H]8O[C@@H](C)[C@H](O)[C@@H](O)[C@H]8O)[C@H](O)[C@H]7O[C@@H]9O[C@@H](C)[C@H](O)[C@@H](O)[C@H]9O CJNUQCDDINHHHD-APRUHSSNSA-N 0.000 claims description 3
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- 238000002360 preparation method Methods 0.000 claims description 3
- 239000000284 extract Substances 0.000 abstract description 10
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- 150000002148 esters Chemical class 0.000 abstract description 4
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- 150000003839 salts Chemical class 0.000 abstract description 4
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- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 description 6
- 230000000694 effects Effects 0.000 description 5
- 208000010228 Erectile Dysfunction Diseases 0.000 description 4
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 4
- XQYZDYMELSJDRZ-UHFFFAOYSA-N papaverine Chemical compound C1=C(OC)C(OC)=CC=C1CC1=NC=CC2=CC(OC)=C(OC)C=C12 XQYZDYMELSJDRZ-UHFFFAOYSA-N 0.000 description 4
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- 229940088597 hormone Drugs 0.000 description 3
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- ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 description 2
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- 231100000872 sexual dysfunction Toxicity 0.000 description 2
- 230000001568 sexual effect Effects 0.000 description 2
- BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 229960003604 testosterone Drugs 0.000 description 2
- MUKYLHIZBOASDM-UHFFFAOYSA-N 2-[carbamimidoyl(methyl)amino]acetic acid 2,3,4,5,6-pentahydroxyhexanoic acid Chemical compound NC(=N)N(C)CC(O)=O.OCC(O)C(O)C(O)C(O)C(O)=O MUKYLHIZBOASDM-UHFFFAOYSA-N 0.000 description 1
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- 208000030663 Libido disease Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- QZVCTJOXCFMACW-UHFFFAOYSA-N Phenoxybenzamine Chemical compound C=1C=CC=CC=1CN(CCCl)C(C)COC1=CC=CC=C1 QZVCTJOXCFMACW-UHFFFAOYSA-N 0.000 description 1
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- VBUWHHLIZKOSMS-RIWXPGAOSA-N invicorp Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)C(C)C)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=C(O)C=C1 VBUWHHLIZKOSMS-RIWXPGAOSA-N 0.000 description 1
- 208000017169 kidney disease Diseases 0.000 description 1
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- 239000002858 neurotransmitter agent Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 238000011458 pharmacological treatment Methods 0.000 description 1
- 229960003418 phenoxybenzamine Drugs 0.000 description 1
- MRBDMNSDAVCSSF-UHFFFAOYSA-N phentolamine Chemical compound C1=CC(C)=CC=C1N(C=1C=C(O)C=CC=1)CC1=NCCN1 MRBDMNSDAVCSSF-UHFFFAOYSA-N 0.000 description 1
- 229960001999 phentolamine Drugs 0.000 description 1
- 239000002571 phosphodiesterase inhibitor Substances 0.000 description 1
- 229930008679 prenylflavonoid Natural products 0.000 description 1
- XEYBRNLFEZDVAW-UHFFFAOYSA-N prostaglandin E2 Natural products CCCCCC(O)C=CC1C(O)CC(=O)C1CC=CCCCC(O)=O XEYBRNLFEZDVAW-UHFFFAOYSA-N 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
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- 208000012201 sexual and gender identity disease Diseases 0.000 description 1
- 230000035946 sexual desire Effects 0.000 description 1
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- 229960003310 sildenafil Drugs 0.000 description 1
- 210000000329 smooth muscle myocyte Anatomy 0.000 description 1
- 239000007790 solid phase Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- IMCGHZIGRANKHV-AJNGGQMLSA-N tert-butyl (3s,5s)-2-oxo-5-[(2s,4s)-5-oxo-4-propan-2-yloxolan-2-yl]-3-propan-2-ylpyrrolidine-1-carboxylate Chemical compound O1C(=O)[C@H](C(C)C)C[C@H]1[C@H]1N(C(=O)OC(C)(C)C)C(=O)[C@H](C(C)C)C1 IMCGHZIGRANKHV-AJNGGQMLSA-N 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/29—Berberidaceae (Barberry family), e.g. barberry, cohosh or mayapple
- A61K36/296—Epimedium
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/54—Lauraceae (Laurel family), e.g. cinnamon or sassafras
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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Abstract
Description
11
DESCRIÇÃODESCRIPTION
"FORMULAÇÕES ÚTEIS NO TRATAMENTO DA IMPOTÊNCIA MASCULINA E FEMININA"" USEFUL FORMULATIONS IN THE TREATMENT OF MALE AND FEMALE IMPOTENCE "
DESCRIÇÃO DA INVENÇÃO A presente invenção diz respeito a formulações que são úteis no tratamento de disfunções sexuais masculinas e femininas. \DISCLOSURE OF THE INVENTION The present invention relates to formulations which are useful in the treatment of male and female sexual dysfunctions. \
As disfunções sexuais têm uma importância considerável e constituem o objecto de esforços intensivos de investigação biomédica. De acordo com estatísticas recentes, o problema da impotência nas suas diversas formas (ausência da libido e disfunções erécteis) afecta cerca de 70% da população com uma idade de cerca de 50 anos e mais, 0 grau de impotência nas suas diversas formas varia obviamente quanto à gravidade, especialmente entre as pessoas idosas, onde se encontra frequentemente associado fisiologicamente com outras perturbações tais como doença cardíaca ou renal.Sexual dysfunctions are of considerable importance and are the subject of intensive biomedical research efforts. According to recent statistics, the problem of impotence in its various forms (absence of libido and erectile dysfunctions) affects about 70% of the population with an age of about 50 years and over, the degree of impotence in its various forms obviously varies especially among the elderly, where it is often associated physiologically with other disorders such as heart or kidney disease.
Os fãrmacos presentemente disponíveis para o tratamento de tais disfunções, especialmente a disfunção erêctil, incluem hormonas tais como testosterona, VIP, derivados de prostaglandinas (PGS) , e agentes cardiovasculares tais como papaverina, fenoxibenzamina e fentolamina.Drugs currently available for the treatment of such disorders, especially erectile dysfunction, include hormones such as testosterone, VIP, prostaglandin derivatives (PGS), and cardiovascular agents such as papaverine, phenoxybenzamine and phentolamine.
No entanto, nenhum destes fármacos proporciona uma solução satisfatória e permanente para o problema, devido aos efeitos secundários que eles provocam e à necessidade 2 de uma injecçao intercavernosa ou intrauretral no caso da papaverina e de PGE2, por exemplo.However, none of these drugs provides a satisfactory and permanent solution to the problem because of the side effects they cause and the need for an intercavernous or intraurethral injection in the case of papaverine and PGE2, for example.
Recentemente, desenvolveram-se inibidores de fosfodiesterase cGMP os quais são particularmente úteis para o tratamento da impotência e são activos por via oral. Um destes agentes,, denominado Sildenafil (WO 94/28902), encontra-se já no mercado.Recently, cGMP phosphodiesterase inhibitors have been developed which are particularly useful for the treatment of impotence and are orally active. One such agent, called Sildenafil (WO 94/28902), is already on the market.
Aqui, mais uma vez, no entanto, os efeitos secundários não são de modo nenhum desprezáveis, e sente-se ainda fortemente a necessidade de tratamentos mais seguros e mais eficazes.Here, again, however, side effects are by no means negligible, and there is still a strong need for safer and more effective treatments.
Numerosos produtos de origem natural (principalmente à base de plantas mas. igualmente de animais) encontram-se actualmente a ser estudados por farmacologia moderna, com base em indicações obtidas a partir da medicina tradicional, para a avaliação da base científica possível para a sua utilização empírica.Numerous products of natural origin (mainly herbal but also animal) are currently being studied by modern pharmacology, based on indications obtained from traditional medicine, for the assessment of the possible scientific basis for their use empirical
Estudos bioquímicos demonstraram a grande complexidade dos mecanismos envolvidos nos processos fisiológicos associados com a actividade sexual, tais como a erecção relativa ao pénis e ao clítoris, a lubrificação vaginal, a ejaculação e o orgasmo.Biochemical studies have demonstrated the great complexity of the mechanisms involved in the physiological processes associated with sexual activity, such as penile and clitoral erection, vaginal lubrication, ejaculation and orgasm.
Mediadores tais como óxido nítrico (NO), os factores enzimãticos envolvidos no. metabolismo dos mensageiros cAMP e cGMP, os receptores adrenérgicos das membranas celulares do músculo liso, neurotransmissores dopaminérgicos, e os receptores de PGS ou outras hormonas constituem os alvos possíveis de um tratamento farmacológico para a impotência e outras disfunções sexuais. 3 É obviamente difícil proporcionar uma solução satisfatória para este problema específico, em parte dado que, além dos aspectos puramente bioquímicos e fisiológicos, existem igualmente factores ambientais e fisiológicos que podem complicar ainda o quadro clínico de pacientes que sofrem de perturbações sexuais. 0 pedido de patente de invenção principal EP 1505997 descreve composições farmacêuticas que compreendem: • extractos de Tribulus terrestris, Epimedium koreanum, Cinnamon cassia na razão em peso de 1,5-3,5:1-2:0,1--0,4, respectivamente; e, eventualmente • arginina ou um seu éster, sal ou precursor fisiologicamente equivalente e um portador ou excipientes apropriados para o tratamento de disfunções sexuais masculinas e femininas.Mediators such as nitric oxide (NO), the enzymatic factors involved in. metabolism of cAMP and cGMP messengers, adrenergic receptors of smooth muscle cell membranes, dopaminergic neurotransmitters, and PGS receptors or other hormones are the possible targets of a pharmacological treatment for impotence and other sexual dysfunctions. 3 It is obviously difficult to provide a satisfactory solution to this specific problem, partly because, in addition to purely biochemical and physiological aspects, there are also environmental and physiological factors which may further complicate the clinical picture of patients suffering from sexual disorders. EP 1505997 discloses pharmaceutical compositions comprising: extracts of Tribulus terrestris, Epimedium koreanum, Cinnamon cassia in the weight ratio of 1.5-3.5: 1-2: 0.1-0, 4, respectively; and, optionally, arginine or a physiologically equivalent ester, salt or precursor thereof and a carrier or excipients suitable for the treatment of male and female sexual dysfunctions.
Os extractos de Tribulus terrestris, Epimedium koreanum, Cinnamon cassia são conhecidos e são já utilizados^ em alguns tipos de medicina tradicional para fins similares mas não são conhecidas quaisquer associações dos mesmos, especialmente nas razões quantitativas específicas indicadas anteriormente.Extracts of Tribulus terrestris, Epimedium koreanum, Cinnamon cassia are known and are already used in some types of traditional medicine for similar purposes but no associations thereof are known, especially in the specific quantitative ratios indicated above.
Em particular, sabe-se que o extracto de Tribulus terrestris induz a síntese de testosterona, uma hormona responsável pela estimulação do desejo sexual tanto nos homens como nas mulheres; o extracto de Epimedium koreanum, ê rico em flavonóides prenilados, possui um efeito vasodilatador mediado pela libertação de NO, de modo que o 4 extracto exerce uma actividade vasocinêtica sobre as artérias e os arteríolos; e o extracto de Cinnamon cassia estimula indirectamente a libido mediante actuação sobre os receptores da'dopamina relacionados com o prazer.In particular, Tribulus terrestris extract is known to induce the synthesis of testosterone, a hormone responsible for the stimulation of sexual desire in both men and women; the extract of Epimedium koreanum, is rich in prenylated flavonoids, has a vasodilatory effect mediated by NO release, so that the extract exerts vasoclinic activity on the arteries and arterioles; and Cinnamon cassia extract indirectly stimulates libido by acting on pleasure-related receptors of dopamine.
No entanto, os resultados terapêuticos susceptíveis de serem obtidos com as composições de acordo com a presente invenção não podem ser explicados meramente com base na actividade de cada extracto; de facto, verificou-se com surpresa que quando os extractos são associados em razões quantitativas diferentes das indicadas anteriormente, eles permanecem inactivos, e podem inclusivamente agravar a perturbação. Um aumento real da actividade sexual só pode, por consequência, ser Obtida pela utilização dos extractos das diversas. plantas numa razão precisa que aumenta tanto o libido como o fornecimento de sangue aos órgãos genitais. A arginina, o seu sal, éster ou precursor, quando utilizada, encontra-se presente em uma razão quantitativa compreendida entre 0,5 e 1,5, de preferência igual a 1, em relação aos extractos das plantas. O pedido de patente de invenção principal EP 1505997 refere-se igualmente à utilização de extractos de Tribulus texrestris, Epimedium koxeanum e Cinnamon cassia na razão em peso de 1,5-3,5 : 1-2 : 0,1-0,4, respectivamente, e eventualmente arginina ou os seus ésteres, sais ou precursores fisiologicamente equivalentes, para preparar medicamentos para o tratamento de disfunções sexuais masculinas e femininas, e especialmente para o tratamento da impotência, de disfunções erécteis, de perturbações do libido, da frigidez e da anorgasmia.However, the therapeutic results obtainable with the compositions according to the present invention can not be explained merely on the basis of the activity of each extract; in fact, it has been found with surprise that when the extracts are associated in quantitative ratios different from those indicated above, they remain inactive, and may even aggravate the disturbance. A real increase in sexual activity can therefore only be obtained by the use of extracts from the various. plants in a precise ratio that increases both libido and blood supply to the genitals. Arginine, its salt, ester or precursor, when used, is present in a quantitative ratio between 0.5 and 1.5, preferably equal to 1, relative to the plant extracts. The main application EP 1505997 also relates to the use of extracts of Tribulus texrestris, Epimedium koxeanum and Cinnamon cassia in the weight ratio of 1.5-3.5: 1-2: 0.1-0.4 , respectively, and optionally arginine or its physiologically equivalent esters, salts or precursors, to prepare medicaments for the treatment of male and female sexual dysfunctions, and especially for the treatment of impotence, erectile dysfunction, libido disorders, frigidity, and of anorgasmia.
Verificou-se agora que, como uma alternativa aos extractos das plantas, podem utilizar-se os ingredientes 5 activos isolados correspondentes, designadamente uma associação de dioscina, icarina e aldeído cinâmico. A utilização da referida associação para a preparação de um mediamento para o tratamento da impotência, da disfunção eréctil, das perturbações do libido, da frigidez e da anorgasmia e igualmente dos medicamentos que compreendem a referida associação constituem ainda objecto da presente invenção.It has now been found that, as an alternative to plant extracts, the corresponding isolated active ingredients, namely an association of dioscin, icarin and cinnamic aldehyde, may be used. The use of said combination for the preparation of a medicament for the treatment of impotence, erectile dysfunction, disorders of libido, frigidity and anorgasmia and also of medicaments comprising said association are still object of the present invention.
As composições de acordo com a presente invenção devem ser tomadas cronicamente, não quase imediatamente antes do intercurso sexual, muito embora em alguns indivíduos a resposta tenha lugar no primeiro tratamento, no decurso de 30 minutos após a tomada do fãrmaco. A administração crónica das composições de acordo com a presente invenção não provoca quaisquer efeitos secundários significativos, é bem tolerada, e não altera os delicados equilíbrios hormonais, especialmente o equilíbrio androgênio/estrogénio, que governam os acontecimentos fisiológicos principais nos homens e nas mulheres tais como a andropausa e a menopausa.The compositions according to the present invention should be taken chronically, not nearly immediately prior to intercourse, although in some individuals the response takes place in the first treatment within 30 minutes of taking the drug. Chronic administration of the compositions according to the present invention does not cause any significant side effects, is well tolerated, and does not alter the delicate hormonal balance, especially androgen / estrogen balance, which governs the major physiological events in men and women such as andropause and menopause.
Exemplos de formas de administração apropriadas das composições de acordo com a presente invenção incluem comprimidos, cápsulas de gelatina mole e dura, supositórios e preparações bebíveis que. contêm uma quantidade eficaz de dioscina, icarina e aldeído cinâmico e um portador ou veículo apropriado. As formulações em fase sólida tais como comprimidos, de libertação não modificada ou gastro--resistentes ou formas líquidas bebíveis são particularmente prefer.idas.Examples of suitable forms of administration of the compositions according to the present invention include tablets, hard and soft gelatin capsules, suppositories and drinkable preparations which. contain an effective amount of dioscin, icarin and cinnamic aldehyde and an appropriate carrier or vehicle. Solid phase formulations such as tablets, non-modified or gastro-resistant release or drinkable liquid forms are particularly preferred.
Lisboa, 9 de Janeiro de 2008Lisbon, January 9, 2008
Claims (2)
Applications Claiming Priority (1)
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| IT2002MI000994A ITMI20020994A1 (en) | 2002-05-10 | 2002-05-10 | USEFUL FORMULATIONS IN THE TREATMENT OF MALE AND FEMALE IMPOTENCE |
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| PT03749863T PT1505997E (en) | 2002-05-10 | 2003-05-02 | UTILIZATION FORMULATIONS IN MALE AND FEMALE IMPOTENCE TREATMENT |
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| KR100692174B1 (en) * | 2005-03-25 | 2007-03-09 | 손병국 | Health functional food having an energetic and sturdy action |
| CN1989990B (en) * | 2005-12-27 | 2010-09-01 | 郭凯 | Medicine for treating erection dysfunction and preparation method thereof |
| EP2011496A1 (en) * | 2007-07-03 | 2009-01-07 | Indena S.P.A. | Combinations of vasoactive substances with estrogens and their use in the treatment of female sexual dysfunctions |
| US20100178413A1 (en) * | 2008-12-17 | 2010-07-15 | Mark Gorris | Food-based Supplement Delivery System |
| US9918489B2 (en) * | 2008-12-17 | 2018-03-20 | Mark Gorris | Food-based supplement delivery system |
| US20110206788A1 (en) * | 2010-01-29 | 2011-08-25 | Chaudhary Latha | Novel herbal composition |
| CN102612370B (en) * | 2009-09-17 | 2014-10-29 | 特拉达药物有限公司 | dietary supplement stimulating the male sexual function |
| ITRM20100068A1 (en) * | 2010-02-19 | 2011-08-20 | Fabrizio Iacono | FOOD SUPPLEMENT WITH COMPONENTS THAT STIMULATE SEXUAL FUNCTION IN THE MALE |
| IT1395768B1 (en) * | 2009-09-17 | 2012-10-19 | Iacono | FOOD SUPPLEMENT WITH COMPONENTS THAT STIMULATE SEXUAL FUNCTION IN THE MALE |
| ES2386859B1 (en) * | 2011-02-07 | 2013-03-22 | Eduardo Antonio Gómez De Diego | NATURAL COMPOSITION TO INCREASE VIGOR. |
| RU2458537C1 (en) * | 2011-03-14 | 2012-08-20 | Общество С Ограниченной Ответственностью "Парафарм" | Biologically active food additive for prevention of men's erectile dysfunction |
| KR20130032419A (en) * | 2011-09-23 | 2013-04-02 | 씨제이제일제당 (주) | Composition comprising the extract of mixed herbs for preventing and improving impotence |
| WO2013106647A1 (en) * | 2012-01-13 | 2013-07-18 | Dharma Biomedical, Llc | Supercritical guggul extracts and uses thereof |
| RU2496491C1 (en) | 2012-08-20 | 2013-10-27 | Общество С Ограниченной Ответственностью "Парафарм" | Method for sexual interest (libido) recovery in males by prescribing dietary supplements for sexual interest (libido) recovery in males |
| TW201420745A (en) * | 2012-11-26 | 2014-06-01 | Tian-De Li | Compound essence oil for enlarging male cavernous body |
| CN103250851A (en) * | 2013-02-24 | 2013-08-21 | 沈根林 | Traditional Chinese medicine kidney invigorating preserved fruit sausage |
| CN103250852A (en) * | 2013-02-24 | 2013-08-21 | 沈根林 | Traditional Chinese medicine kidney invigorating preserved fruit sausage |
| CN104000198B (en) * | 2014-06-13 | 2016-03-23 | 上海赫尔伯生物科技有限公司 | A kind of have kidney tonifying, essence replenishing, the emerging positive compound capsule acted on of benefit god and preparation method thereof |
| CN104352540B (en) * | 2014-10-20 | 2017-08-18 | 成都中医药大学 | It is a kind of to treat hydrogel matrix type sustained release tablets of coronary disease and angina pectoris and preparation method thereof |
| US20190105274A1 (en) * | 2015-07-13 | 2019-04-11 | Kyowa Hakko Bio Co., Ltd. | Tablets containing arginine at high concentration |
| CN106614589A (en) * | 2016-11-13 | 2017-05-10 | 徐州得铸生物科技有限公司 | Insecticide composition containing tribulus terrestris saponins |
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| KR0148511B1 (en) * | 1993-09-14 | 1998-11-02 | 최형기 | Pharmaceutical composition for prophylaxis and treatment of sexual nervous hyper sensitivity |
| FR2765483B1 (en) * | 1997-07-04 | 2000-02-04 | Philippe Gorny | MEDICINE FOR TREATING ERECTILE DYSFUNCTIONS |
| US6007824A (en) * | 1998-07-09 | 1999-12-28 | Duckett; Melvin J. | Natural composition and method for the treatment of sexual dysfunction |
| US20020013280A1 (en) * | 2000-06-16 | 2002-01-31 | Zhongcheng Xin | Pharmaceutical composition for preventing and treating sexual dysfunction and vasculargenic disease comprising icariin |
| KR100394329B1 (en) * | 1999-06-17 | 2003-08-09 | 북경동방백오의약개발유한공사 | Pharmaceutical composition for treating sexual dysfunction and vasculagenic disease |
| US6702733B1 (en) * | 1999-07-01 | 2004-03-09 | 40 J's Llc | Expanded clitoral sensitizing compounds with methods and apparatus for the delivery of these compounds |
| KR20010009653A (en) * | 1999-07-12 | 2001-02-05 | 유제경 | Composition for treating sexual dysfunction |
| US20010008638A1 (en) * | 1999-07-14 | 2001-07-19 | Brian J. Wilding | Nutritional supplement comprising at least one prohormone and at least one anti-estrogen compound in a time-release dosage form |
| US6343258B1 (en) * | 1999-08-13 | 2002-01-29 | ALEXIS Brian | Method for testing for readiness for harvesting of tribulus terrestris l. having high steroidal saponin content |
| US6399579B1 (en) * | 2000-08-15 | 2002-06-04 | Hauser, Inc. | Compositions comprising icariside I and anhydroicaritin and methods for making the same |
| US6803060B2 (en) * | 2000-09-07 | 2004-10-12 | Joe Reyes | Composition to boost libido |
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